Kinetic interactions between 4-methylpyrazole and ethanol in healthy humans

Alcoholism: Clinical and Experimental Research

Volumn 20, Issue 5, 1996, Pages 804-809

  Jacobsen, D ^a   Sebastian, C S ^a   Dies, D F ^a   Breau, R L ^a   Spann, E G ^a   Barron, S K ^a   McMartin, K E ^a  

^a LOUISIANA STATE UNIV MEDICAL CENTER   (United States)

Author keywords

Alcohol Dehydrogenase; Cytochrome P 450; Drug Metabolism; Ethylene Glycol Poisoning; Methanol Poisoning

Indexed keywords

4 METHYLPYRAZOLE; ALCOHOL DEHYDROGENASE; CYTOCHROME P450; ETHYLENE GLYCOL;

ARTICLE; CLINICAL TRIAL; CROSSOVER PROCEDURE; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG ELIMINATION; DRUG PROTEIN BINDING; ENZYME ACTIVITY; HUMAN; HUMAN EXPERIMENT; INTRAVENOUS DRUG ADMINISTRATION; LIVER MICROSOME METABOLISM; MALE; METHANOL POISONING; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL;

EID: 0029812026     PISSN: 01456008     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1530-0277.1996.tb05255.x     Document Type: Article

References (31)

1. Jacobsen D, McMartin KE: Methanol and ethylene glycol poisonings: Mechanism of toxicity, clinical course, diagnosis and treatment. Med Toxicol 1:309-334, 1986
2. Baud FJ, Bismuth C, Gamier R, Galliot M, Astier A, Maistre G, Soffer M: 4-Methylpyrazole may be an alternative to ethanol therapy for ethylene glycol intoxication in man. J Toxicol Clin Toxicol 24:463-483, 1987
3. Baud FJ, Galliot M, Astier A, et al: Treatment of ethylene glycol poisoning with intravenous 4-methylpyrazole. N Engl J Med 319:97-100, 1988
4. Li TK, Theorell H: Human liver alcohol dehydrogenase: Inhibition by pyrazole and pyrazole analogs. Acta Chem Scand 23:892-902, 1969
5. McMartin KE, Hedstrom KG, Tolf BR, Ostling-Wintzell H, Blomstrand R: Studies on the metabolic interactions between 4-methylpyrazole and methanol using the monkey as an animal model. Arch Biochem Biophys 199:606-614, 1980
6. McMartin KE, Collins TD: Distribution of oral 4-methylpyrazole in the rat: Inhibition of elimination by ethanol. J Toxicol Clin Toxicol 26:451-466, 1988
7. Jacobsen D, Sebastian S, Blomstrand R, McMartin KE: 4-Methylpyrazole: A controlled study of safety in healthy human subjects after single, ascending doses. Alcohol Clin Exp Res 12:516-522, 1988
8. Jacobsen D, Barron SK, Sebastian CS, Blomstrand R, McMartin KE: Non-linear kinetics of 4-methylpyrazole in healthy human subjects. Eur J Clin Pharmacol 37:599-604, 1989
9. Jacobsen D, Sebastian CS, Barron SK, Carriere EW, McMartin KE: Effects of 4-methylpyrazole, methanol/ethylene glycol antidote, in healthy humans. J Emerg Med 8:455-461, 1990
10. Fujimiya T, Yamika K, Fukui Y: Parallel first-order and Michaelis-Menten elimination kinetics of ethanol. Respective role of alcohol dehydrogenase (ADH), non-ADH and first-order pathways. J Pharmacol Exp Ther 249:311-317, 1989
11. Blomstrand R, Ellin A, Lof A, Ostling-Wintzell H: Biological effects and metabolic interactions after chronic and acute administration of 4-methylpyrazole and ethanol to rats. Arch Biochem Biophys 199:591-605, 1980
12. Baker RN, Alenty AL, Zack JF Jr: Simultaneous determination of lower alcohols, acetone and acetaldehyde in blood by gas chromatography. J Chromatogr Sci 7:312-314, 1969
13. McMartin KE, Collins TD, Hewlett TP: High pressure liquid Chromatographic assay of 4-methylpyrazole. Measurements of plasma and urine levels. J Toxicol Clin Toxicol 22:133-148, 1984
14. Diczfalusy U, Eklöf R: Determination of 4-methylpyrazole in plasma using solid phase extraction and HPLC. Biomed Chromatogr 2:226-227, 1988
15. Murphy RC, Watkins WD: Pharmacology of pyrazoles. I. Structure elucidation of metabolites of 4-methylpyrazole. Biochem Biophys Res Commun 49:283-291, 1972
16. Blomstrand R, Ohman G: Studies on the metabolites of the ADH inhibitor 4-methylpyrazole in the rat. Life Sci 13:107-112, 1973
17. Wilkinson PK: Pharmacokinetics of ethanol: A review. Alcohol Clin Exp Res 4:6-21, 1980
18. Rangno RE, Kreeft JH, Sitar DS: Ethanol 'dose-dependent' elimination: Michaelis-Menten K classical kinetic analysis. Br J Clin Pharmacol 12:667-673, 1981
19. Tzamaloukas AH, Eschbach RC, Jackson JE, Long DA: Equilibration, distribution, and elimination of a single dose of intravenous ethanol in dogs with intact renal function or anuria. Alcohol Clin Exp Res 10:293-299, 1986
20. Blomstrand R, Theorell H: Inhibitory effects on ethanol oxidation in man after administration of 4-methylpyrazole. Life Sci 9:631-640, 1970
21. Pietruszko R: Human liver alcohol dehydrogenase - Inhibition of methanol activity by pyrazole, 4-methylpyrazole, 4-hydroxy-methylpyrazole and 4-carboxypyrazole. Biochem Pharmacol 24:1603-1607, 1975
22. Teschke R, Matsuzaki S, Ohnishi K, DeCarli LM, Lieber CS: Microsomal ethanol oxidizing system (MEOS): Current status of its characterization and its role. Alcohol Clin Exp Ther 1:7-15, 1977
23. Eisenga BH, Collins TD, McMartin KE: Differential effects of acute ethanol on urinary excretion of folate derivatives in the rat. J Pharmacol Exp Ther 248:916-922, 1989
24. Feiermann DE, Cederbaum AI: Interaction of pyrazole and 4-methylpyrazole with hepatic microsomes: Effect on cytochrome P-450 content, microsomal oxidation of alcohols and binding spectra. Alcohol Clin Exp Res 9:421-428, 1985
25. Feiermann DE, Cederbaum AI: Increased content of cytochrome P-450 and 4-methylpyrazole binding spectra after 4-methylpyrazole treatment. Biochem Biophys Res Commun 126:1076-1081, 1985
26. Muhoberac BB, Roberts RK, Hoyumpa AM, Schenker S: Mechanism(s) of ethanol-drug interaction. Alcohol Clin Exp Res 8:583-593, 1984
27. Winters DK, Cederbaum AI: Time course characterization of the induction of cytochrome P-450 2E1 by pyrazole and 4-methylpyrazole. Biochem Biophys Acta 1117:15-24, 1992
28. Jacobsen D, Frederichsen PF, Knutsen KM, Sorum Y, Talseth T, Odegaard OR: A prospective study of 1212 cases of acute poisoning. General epidemiology. Hum Toxicol 3:93-106, 1984
29. Jacobsen D, Jansen H, Wiik-Larsen E, Bredesen JE, Halvorsen S: Studies on methanol poisoning. Acta Med Scand 212:5-10, 1982
30. Jacobsen D, Ostby N, Bredesen JE: Studies on ethylene glycol poisoning. Acta Med Scand 212:11-15, 1982
31. Mayersohn MI, Owens SM, Anaya AL, Bliss M, Achari R: 4-Methylpyrazole disposition in the dog: Evidence for saturable elimination. J Pharmacol Sci 74:895-896, 1985